MEK/PI3K-IN-2

Names

[ CAS No. ]:
2281803-33-4

[ Name ]:
MEK/PI3K-IN-2

Biological Activity

[Description]:

MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> MEK
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

[Target]

MEK1:352 ± 2 nM (IC50)

PI3Kα:107 ± 21 nM (IC50)

PI3Kδ:137 ± 7 nM (IC50)

PI3Kγ:2567 ± 364 nM (IC50)

PI3Kβ:3880 ± 725 nM (IC50)


[References]

[1]. Van Dort ME, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

Chemical & Physical Properties

[ Molecular Formula ]:
C38H41F5IN9O7

[ Molecular Weight ]:
957.68

Related Compounds